Vatalanib (Synonyms: PTK787; ZK-222584; CGP-79787)

Name: Vatalanib
Brand: MedChemExpress
SKU: HY-10203
Rating: 5.0 (13 reviews)

Cat. No.: HY-10203 Purity: 99.93%: FAQs
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Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC₅₀ of 37 nM.

For research use only. We do not sell to patients.

Vatalanib Chemical Structure

CAS No. : 212141-54-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 145	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
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Based on 13 publication(s) in Google Scholar

Other Forms of Vatalanib:

13 Publications Citing Use of MCE Vatalanib

•Kitazato Graduate School of Pharmaceutical Sciences. Kitasato University. 2017.

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View All VEGFR Isoform Specific Products:

View All Isoforms

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC₅₀ of 37 nM.

IC₅₀ & Target^[1]

VEGFR2

37 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	21.16 μM Compound: 8; PTK787	Inhibition of human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Inhibition of human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 26590508]
A549	IC₅₀	21.16 μM Compound: PTK-787	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 20537434]
CHO	IC₅₀	0.016 μM Compound: A, PTK-787	Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA	[PMID: 19124243]
EA.hy 926	IC₅₀	19.98 μM Compound: 1	Cytotoxicity against human EAhy926 cells assessed as reduction in cell viability after 72 hrs by presto-blue assay Cytotoxicity against human EAhy926 cells assessed as reduction in cell viability after 72 hrs by presto-blue assay	[PMID: 30776229]
EA.hy 926	IC₅₀	22.32 μM Compound: Vatalanib	Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 72 hrs by PrestoBlue reagent based assay Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 72 hrs by PrestoBlue reagent based assay	[PMID: 34459195]
HEK293	IC₅₀	0.021 μM Compound: A, PTK-787	Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA	[PMID: 19124243]
HEK293	IC₅₀	0.021 μM Compound: A	Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA	[PMID: 16460936]
HT-29	IC₅₀	22.11 μM Compound: 8; PTK787	Inhibition of human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Inhibition of human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 26590508]
HT-29	IC₅₀	22.11 μM Compound: PTK-787	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 20537434]
HUVEC	IC₅₀	33 nM Compound: 1, PTK-787	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay	[PMID: 21247763]
HUVEC	IC₅₀	33 nM Compound: 1, PTK-787	Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay	[PMID: 21074435]
MDA-MB-231	IC₅₀	57.72 μM Compound: 8; PTK787	Inhibition of human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Inhibition of human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 26590508]
MDA-MB-231	IC₅₀	57.72 μM Compound: PTK-787	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 20537434]
PBMC	IC₅₀	> 1 μM Compound: 17 (PTK-787)	In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay	[PMID: 16107139]

In Vitro

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC₅₀ of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC₅₀ of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors^[1]. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

346.81

Formula

C₂₀H₁₅ClN₄

CAS No.

212141-54-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(C=C1)NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (180.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8834 mL	14.4171 mL	28.8342 mL
5 mM	0.5767 mL	2.8834 mL	5.7668 mL
10 mM	0.2883 mL	1.4417 mL	2.8834 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (252 KB) HNMR (314 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Wood JM, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000, 60(8 [Content Brief]

[2]. Murakami M, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011, 18(2), 589-596. [Content Brief]

[3]. Wan J, et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308. [Content Brief]

Kinase Assay ^[1]	Each GST-fused kinase is incubated under optimized buffer conditions. ATP in a total volume of 30 μL in the presence or absence of a test substance (Vatalanib) for 10 min at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin. After 24 h, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of Vatalanib. As a control, wells without growth factor are also included. After 24 h of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3' 5,5'-tetramethylbenzidine substrate^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	A porous Teflon chamber (volume, 0.5 mL) is filled with 0.8% w/v agar containing heparin (20 units/mL) with or without growth factor (3 μg/mL human VEGF, 2 μg/mL human PDGF) is implanted s.c. on the dorsal flank of C57/C6 mice. The mice are treated with Vatalanib (12.5, 25 or 50 mg/kg dihydrochloride p.o. once daily) or vehicle (water) starting 1 day before implantation of the chamber and continuing for 5 days after. At the end of treatment, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is carefully removed and weighed, and the blood content is assessed by measuring the hemoglobin content of the tissue^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wood JM, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000, 60(8 [Content Brief] [2]. Murakami M, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011, 18(2), 589-596. [Content Brief] [3]. Wan J, et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8834 mL	14.4171 mL	28.8342 mL	72.0856 mL
	5 mM	0.5767 mL	2.8834 mL	5.7668 mL	14.4171 mL
	10 mM	0.2883 mL	1.4417 mL	2.8834 mL	7.2086 mL
	15 mM	0.1922 mL	0.9611 mL	1.9223 mL	4.8057 mL
	20 mM	0.1442 mL	0.7209 mL	1.4417 mL	3.6043 mL
	25 mM	0.1153 mL	0.5767 mL	1.1534 mL	2.8834 mL
	30 mM	0.0961 mL	0.4806 mL	0.9611 mL	2.4029 mL
	40 mM	0.0721 mL	0.3604 mL	0.7209 mL	1.8021 mL
	50 mM	0.0577 mL	0.2883 mL	0.5767 mL	1.4417 mL
	60 mM	0.0481 mL	0.2403 mL	0.4806 mL	1.2014 mL
	80 mM	0.0360 mL	0.1802 mL	0.3604 mL	0.9011 mL
	100 mM	0.0288 mL	0.1442 mL	0.2883 mL	0.7209 mL

Vatalanib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vatalanib212141-54-3PTK787 ZK-222584 CGP-79787PTK 787PTK-787ZK222584ZK 222584ZK-222584CGP79787CGP 79787CGP-79787VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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Vatalanib (Synonyms: PTK787; ZK-222584; CGP-79787)

Customer Review

Other Forms of Vatalanib:

Vatalanib Related Antibodies

13 Publications Citing Use of MCE Vatalanib

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Vatalanib Related Antibodies

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Complete Stock Solution Preparation Table

Vatalanib Related Classifications

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